What Is An Agonist-Antagonist Medicine And When Might I Need It?

Question: What Is An Agonist-Antagonist Medicine And When Is It Used For Pain Relief?

Answer: Agonist-antagonist medicines represent a class of opiod medications that bind to both a receptor that produces pain relief, which is the agonist portion, and bind to another receptor that does not produce a physiological effect, which is the antagonist portion.

The stimulus for the development of mixed agonist-antagonist drugs stemmed from the desire to have pain relievers like opiods with less respiratory depression and addictive potential. Some examples of these drugs are pentazocine or Talwin, nalbuphine or Nubain, and butorphanol or Stadol.

Clinically, these medicines are used less often than opiods like morphine, oxycodone, fentanyl, and methadone because they have more limited pain-relieving effects and undesirable side effects. Buprenorphine or Buprenex is another example of a mixed agonist-antagonist medicine that is growing in use due to its ability to produce good pain relief, its potential for reduced risk of respiratory depression, and its ability for use as a maintenance drug for opioid-dependent patients.

Some physicians prescribe agonist-antagonist medicines when your pain is mild or moderate in severity and then move to more powerful agents if your pain escalates in intensity.